title: Synthesis and biological activity evaluation of 5-pyrazoline substituted 4-thiazolidinones.
abstract: A series of novel 5-pyrazoline substituted 4-thiazolidinones have been synthesized. Target compounds were evaluated for their anticancer activity in vitro within DTP NCI protocol. Among the tested compounds, the derivatives 4d and 4f were found to be the most active, which demonstrated certain sensitivity profile toward the leukemia subpanel cell lines with GI₅₀ value ranges of 2.12-4.58 μM (4d) and 1.64-3.20 μM (4f). The screening of antitrypanosomal and antiviral activities of 5-(3-naphthalen-2-yl-5-aryl-4,5-dihydropyrazol-1-yl)-thiazolidine-2,4-diones was carried out with the promising influence of the mentioned compounds on Trypanosoma brucei, but minimal effect on SARS coronavirus and influenza types A and B viruses.
authors.affiliation: Department of Pharmaceutical, Organic and Bioorganic Chemistry, Danylo Halytsky Lviv National Medical University, Pekarska 69, Lviv 79010, Ukraine.
authors.forename: Dmytro
authors.initials: D
authors.lastname: Havrylyuk
authors.forename: Borys
authors.initials: B
authors.lastname: Zimenkovsky
authors.forename: Olexandr
authors.initials: O
authors.lastname: Vasylenko
authors.forename: Craig W
authors.initials: CW
authors.lastname: Day
authors.forename: Donald F
authors.initials: DF
authors.lastname: Smee
authors.forename: Philippe
authors.initials: P
authors.lastname: Grellier
authors.forename: Roman
authors.initials: R
authors.lastname: Lesyk
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D060326:Chemistry Techniques, Synthetic; D006801:Humans; D011720:Pyrazoles / Q000737:chemistry*; D013329:Structure-Activity Relationship; D053778:Thiazolidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects; D014780:Viruses / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D000981:Antiprotozoal Agents; D000998:Antiviral Agents; D011720:Pyrazoles; D053778:Thiazolidines
keywords: 4-Thiazolidinones; Anticancer activity; Antitrypanosomal activity; Antiviral activity; Pyrazolines; Synthesis